AR103866A2 - Composición farmacéutica para la inhibición de la actividad cinasa her-2, compuesto, formas cristalinas aisladas de monohidrato de maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida, maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro y maleato parcialmente hidratado de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida y métodos para preparar (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida como una sal de maleato y maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro - Google Patents
Composición farmacéutica para la inhibición de la actividad cinasa her-2, compuesto, formas cristalinas aisladas de monohidrato de maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida, maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro y maleato parcialmente hidratado de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida y métodos para preparar (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida como una sal de maleato y maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidroInfo
- Publication number
- AR103866A2 AR103866A2 ARP160100590A ARP160100590A AR103866A2 AR 103866 A2 AR103866 A2 AR 103866A2 AR P160100590 A ARP160100590 A AR P160100590A AR P160100590 A ARP160100590 A AR P160100590A AR 103866 A2 AR103866 A2 AR 103866A2
- Authority
- AR
- Argentina
- Prior art keywords
- butenamide
- anilino
- piridinylmetoxi
- quinolinil
- etoxi
- Prior art date
Links
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 title abstract 6
- 150000002688 maleic acid derivatives Chemical class 0.000 title abstract 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- HSMPSHPWCOOUJH-UHFFFAOYSA-N anilinyl Chemical compound [NH]C1=CC=CC=C1 HSMPSHPWCOOUJH-UHFFFAOYSA-N 0.000 title 5
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 title 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 title 1
- 239000002131 composite material Substances 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- JWNPDZNEKVCWMY-VQHVLOKHSA-N neratinib Chemical compound C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 JWNPDZNEKVCWMY-VQHVLOKHSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 102000001301 EGF receptor Human genes 0.000 abstract 1
- 108060006698 EGF receptor Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000011976 maleic acid Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/145—Maleic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Las formas de sal de maleato de (E)-N-{4-[3-cloro-4-(2-piridinilmetoxi) anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida, métodos para preparar formas de sal de maleato cristalina. Los compuestos asociados, y composiciones farmacéuticas que contienen las sales de maleato. Las sales de maleato son útiles en el tratamiento de cáncer, particularmente aquellos afectados por las cinasas de la familia del receptor del factor de crecimiento epidérmico. Reivindicación 1: Un método para preparar (E)-N-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida como una sal de maleato, caracterizado por comprender la etapa de: mezclar (E)-N-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida y acido maleico en una solución agua-alcohol a una temperatura elevada. Reivindicación 14: Un compuesto caracterizado por pertenecer al conjunto que consiste del grupo de fórmulas (1).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12479607P | 2007-10-17 | 2007-10-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR103866A2 true AR103866A2 (es) | 2017-06-07 |
Family
ID=40347915
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP080104565A AR068932A1 (es) | 2007-10-17 | 2008-10-17 | Metodos para preparar (e) .n-(4-( 3- cloro-4-(2- piridinilmetoxi ) anilino )-3- ciano-7-etoxi-6 quinolinil) -4 - (dimetilamino) -2- butenamida como una sal de maleato, composiciones farmaceuticas para la inhibicion de la actividad cinasa her-2 y formas cristalinas aisladas de dichas sales de maleato |
ARP160100590A AR103866A2 (es) | 2007-10-17 | 2016-03-04 | Composición farmacéutica para la inhibición de la actividad cinasa her-2, compuesto, formas cristalinas aisladas de monohidrato de maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida, maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro y maleato parcialmente hidratado de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida y métodos para preparar (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida como una sal de maleato y maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP080104565A AR068932A1 (es) | 2007-10-17 | 2008-10-17 | Metodos para preparar (e) .n-(4-( 3- cloro-4-(2- piridinilmetoxi ) anilino )-3- ciano-7-etoxi-6 quinolinil) -4 - (dimetilamino) -2- butenamida como una sal de maleato, composiciones farmaceuticas para la inhibicion de la actividad cinasa her-2 y formas cristalinas aisladas de dichas sales de maleato |
Country Status (21)
Country | Link |
---|---|
US (6) | US8022216B2 (es) |
EP (6) | EP2212311A2 (es) |
JP (10) | JP2011500712A (es) |
KR (5) | KR20130025862A (es) |
CN (7) | CN103554086A (es) |
AR (2) | AR068932A1 (es) |
AU (1) | AU2008312474B2 (es) |
BR (2) | BRPI0818464B8 (es) |
CA (2) | CA2702930C (es) |
CL (1) | CL2008003088A1 (es) |
ES (3) | ES2602123T3 (es) |
HK (2) | HK1146405A1 (es) |
IL (3) | IL308687A (es) |
IN (1) | IN2015DN01135A (es) |
MX (4) | MX342681B (es) |
NZ (3) | NZ705641A (es) |
PA (1) | PA8800701A1 (es) |
RU (2) | RU2463300C2 (es) |
SG (2) | SG185312A1 (es) |
TW (1) | TW200934761A (es) |
WO (1) | WO2009052264A2 (es) |
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DE10349113A1 (de) | 2003-10-17 | 2005-05-12 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung von Aminocrotonylverbindungen |
CN108421044A (zh) | 2005-02-03 | 2018-08-21 | 综合医院公司 | 治疗吉非替尼耐药性癌症的方法 |
WO2007056118A1 (en) | 2005-11-04 | 2007-05-18 | Wyeth | Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272 |
US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
EP2310011B1 (en) | 2008-06-17 | 2013-07-24 | Wyeth LLC | Antineoplastic combinations containing hki-272 and vinorelbine |
AU2009279771B2 (en) | 2008-08-04 | 2015-05-14 | Wyeth Llc | Antineoplastic combinations of 4-anilino-3-cyanoquinolines and capecitabine |
KR20220143154A (ko) | 2009-04-06 | 2022-10-24 | 와이어쓰 엘엘씨 | 네라티닙을 이용한 유방암의 치료법 |
ES2660146T3 (es) * | 2009-04-29 | 2018-03-21 | Nerviano Medical Sciences S.R.L. | Sales del inhibidor de cdk |
AU2010315362B2 (en) | 2009-11-09 | 2015-01-22 | Wyeth Llc | Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea |
EP3575413A1 (en) | 2009-12-11 | 2019-12-04 | Wyeth LLC | Phosphatidylinositol-3-kinase pathway biomarkers |
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WO2016210345A1 (en) | 2015-06-25 | 2016-12-29 | The California Institute For Biomedical Research | Composition and methods for inhibiting mammalian sterile 20-like kinase 1 |
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